Abstract: Soft anticholinergic esters of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; R is C1-C8 alkyl, straight or branched chain; and X? is an anion with a single negative charge; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.
Abstract: Compounds of formulae I and II are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and manage serotonin-mediated diseases and disorders:
Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family is disclosed.
Type:
Grant
Filed:
January 14, 2009
Date of Patent:
January 7, 2014
Assignee:
Siga Technologies, Inc.
Inventors:
Dongcheng Dai, Dennis E. Hruby, Tove C. Bolken, Sean M. Amberg, Travis K. Warren
Abstract: The present invention is concerned with a process for preparing compounds of the general formula (I). These compounds can preferably be used to prepare bioactive agents. The reaction of the invention starts from the corresponding hydroxy compounds which are oxidized, with Ru catalysis, in a one-phase aqueous system.
Abstract: New types of derivatives of tris(2-hydroxyphenyl)methanes which have, as functional groups, polyalkoxy groups or polyalkoxy groups modified with terminal hydrophilic groups, preparation of such compounds and their use, especially as surfactants and thickeners.
Type:
Grant
Filed:
May 19, 2011
Date of Patent:
December 31, 2013
Assignee:
BASF SE
Inventors:
Marta Reinoso Garcia, Günter Oetter, Vandana Kurkal-Siebert, Björn Heinz, Christian Bittner, Markus Hansch, Roman Benedikt Raether
Abstract: There is provided a process for the preparation of a compound of formula (7) or salts thereof: wherein R1 represents a hydrogen or a hydrocarbyl group, R2 represents a hydrogen or substituent group, R3 represents a hydrogen or a hydrocarbyl group, and X represents a hydrogen or substituent group which comprises a) cyanating a compound of formula (1): wherein Y represents a halo group, preferably CI or Br; P1 represents hydrogen or a protecting group, and W represents ?O or —OP2, in which P2 represents hydrogen or a protecting group, to give a compound of formula (2): b) reducing the compound of formula (2) to give a compound of formula (3): coupling the compound of formula (3) with a compound of formula (4): to give a compound of formula (5): when W represents —OP2, deprotecting and then oxidizing the compound of formula (5) to give a compound of formula (6): and e) subjecting the compound of formula (5) when W represents ?O, or compound of formula (6) to ring-opening, and removal of any remaining protecting
Type:
Grant
Filed:
August 14, 2008
Date of Patent:
December 24, 2013
Assignee:
Redx Pharma Limited
Inventors:
David John Moody, Jonathan William Wiffen
Abstract: Cinnamic acid-based oligomers and therapeutic uses thereof are provided. The oligomers are used as anti-inflammation agents, inhibitors of elastase and anti-oxidants, and in some cases (e.g. the treatment of lung disorders such as lung cancer) all three activities are simultaneously beneficial. Subsets of the oligomers (e.g. ?-O4 and ?-5 trimers and tetramers) are used as anticoagulants.
Type:
Grant
Filed:
June 25, 2013
Date of Patent:
December 24, 2013
Assignee:
Virginia Commonwealth University
Inventors:
Umesh R. Desai, Brian L. Henry, Aiye Liang, Jay Thakkar, John B. Mangrum, Ivo Torres Filho, Bruce D. Spiess, Masahiro Sakagami, Bhawana Saluja
Abstract: The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.
Type:
Grant
Filed:
July 1, 2011
Date of Patent:
December 17, 2013
Assignee:
Furiex Pharmaceuticals, Inc.
Inventors:
Luigi Anzalone, Frank J. Villani, Christopher A. Teleha, Penina Feibush, Barry Fegely
Abstract: The invention relates to a method for producing 6-chlorodibenzo[d,f][1,3,2]-dioxaphosphepin (formula 1), comprising the following steps: a) addition of liquid 2,2?-dihydroxybiphenyl into a reactor to an excess of phosphorous trichloride under inert gas and stirring; b) discharge and neutralization of the resulting gases from the reaction mixture; c) separation of the excess phosphorous trichloride; d) obtention of 6-chlorodibenzo[d,f][1,3,2]-dioxaphosphepin.
Type:
Grant
Filed:
October 9, 2009
Date of Patent:
December 17, 2013
Assignee:
Evonik Oxeno GmbH
Inventors:
Dirk Fridag, Robert Franke, Bernhard Schemmer, Burkard Kreidler, Bjoern Wechsler
Abstract: Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
Abstract: Claimed are unsymmetrical Pyrrolobenzodiazepine-dimers (PBD-dimers) of formula (I), that are unsymmetrical due at least to the values that the variables R12 and R2 represent. Formula (I), wherein: R2 is of formula (II), where A is a C5-7 aryl group, X is selected from the group comprising: OH, SH, CO2H, COH, N?C?O, NHRN, wherein RN is selected from the group comprising H and C1-4 alkyl, and (OC2H4)mOCH3, where m is 1 to 3, and either: (i) Q1 is a single bond, and Q2 is selected from a single bond and —Z—(CH2)n—, where Z is selected from a single bond, O, S and NH and n is from 1 to 3; or (ii) Q1 is —CH?CH—, and Q2 is a single bond; R12 is a C5-10 aryl group, optionally substituted by one or more substituents selected from the group comprising: halo, nitro, cyano, ether, C1-7 alkyl, C3-7 heterocyclyl and bis-oxy-C1-3 alkylene. The other variables are as defined in the claims. The compounds are useful for the treatment of proliferative diseases.
Type:
Grant
Filed:
October 16, 2009
Date of Patent:
November 26, 2013
Assignee:
Spirogen Sarl
Inventors:
Philip Wilson Howard, Stephen John Gregson, Luke Masterson
Abstract: The present invention relates to a process for the regioselective synthesis of 1-alkyl-3-halo-alkylpyrazole-4-carboxylic acid derivatives by cyclization of 2,3-disubstituted acrylic acid derivatives, and to the hydrazones formed as intermediates in the process.
Type:
Grant
Filed:
March 14, 2013
Date of Patent:
November 26, 2013
Assignee:
Bayer Intellectual Property GmbH
Inventors:
Sergii Pazenok, Norbert Lui, Jens-Dietmar Heinrich, Thomas Wollner
Abstract: Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed in connection with modification of procaspases such as procaspase-3. In embodiments, compositions are capable of activation of procaspase-3.
Type:
Grant
Filed:
April 15, 2011
Date of Patent:
November 26, 2013
Assignee:
The Board of Trustees of the of The University of Illinois
Inventors:
Paul J. Hergenrother, Karson S. Putt, Quinn P. Peterson, Valerie Fako
Abstract: A process for preparing 3-amino-3-cyclobutylmethyl-2-hydroxypropionamide of the Formula I: or a salt thereof involves providing a compound of the Formula VI described herein in a solution comprising predominately dimethylsulfoxide (DMSO) and converting this compound directly to the compound of the Formula VIII described herein without working up or isolating the intermediate compound of the Formula VII described herein.
Type:
Grant
Filed:
December 17, 2008
Date of Patent:
November 19, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Shuan Dong, Jeonghan Park, Eugene John Vater
Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.
Abstract: Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.
Abstract: The invention relates to aryl-substituted polycyclic amines of formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof; where the symbols and radicals are explained in the description, as well as to pharmaceutical compositions containing them and to methods of treatment using them.
Type:
Grant
Filed:
July 29, 2010
Date of Patent:
November 19, 2013
Assignee:
Sanofi-Aventis Deutschland GmbH
Inventors:
Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Gerhard Hessler, Petra Lennig
Abstract: Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38?, and p38? kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.
Type:
Grant
Filed:
February 25, 2013
Date of Patent:
November 12, 2013
Assignee:
Novartis AG
Inventors:
Hengyuan Lang, Olga M. Fryszman, Edcon Chang, Jiong Lan, Yunfeng Fang
Abstract: The present invention relates to a method of preparing a nitrogen-doped graphene comprising preparing a Edge-Functionalized Graphene by binding a graphite with a organic material having amino groups and functional groups such as carboxy acid group through an electrophilic substitution reaction, and heat treating the resultant Edge-Functionalized Graphene, and a nitrogen-doped graphene prepared thereby. According to the present invention, by a more inexpensive and simpler method, a nitrogen-doped graphene can be prepared at higher purity and higher yield. The nitrogen-doped graphene obtained by the present invention has very excellent physical and electric properties, and particularly has a superior oxygen reduction capability, compared with the platinum catalyst used at cathode of a H2/O2 fuel cell so that it will replace the platinum to lower more the cost of a H2/O2 fuel cell or to increase its life and further to provide a new turning point for the commercialization of a H2/O2 fuel cell.
Type:
Grant
Filed:
March 31, 2011
Date of Patent:
November 5, 2013
Assignee:
Unist Academy-Industry Research Corporation
Abstract: The present invention relates to a compound represented by the formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a medicament containing the same. The compound represented by the formula (I) has an ability to bind to an S1P receptor (particularly, EDG-1, EDG-6, and/or EDG-8) and is useful for preventing and/or treating for rejection to transplantation, graft-versus-host disease, autoimmune diseases, allergic diseases, neurodegenerating diseases, and the like. wherein all symbols are described in the specification.